The ability to prepare functionalized organic molecules rationally and predictably, whether individually or in libraries is central to organic synthesis, medicinal chemistry and the pharmaceutical industry. The aims of this work are to develop new and/or improved methods for the formation of carbon-nitrogen and carbon- oxygen bonds and to apply this chemistry for the preparation of a variety of medicinally interesting compounds. Included in this work is the development of new strategies and techniques for the preparation of heterocyclic compounds, which are the building blocks of medicinal chemistry and the pharmaceutical industry. Further, information gained from this work will help to understand the mechanism of the processes that are being developed in order to increase the rate of improvement of the techniques that we are studying. The development of new methods for organic synthesis is key to the development of the field of organic chemistry as a whole. The methods for carbon-nitrogen and carbon-oxygen bond formation, described herein, are regularly used by those in the pharmaceutical industry for the preparation of analogues with increased potency and reduced side effects. Moreover, the methods can be employed for the preparation of quantities of new substances for preclinical and clinical testing and for the actual manufacture of a pharmaceutical agent. The techniques that are being developed allow for these important functions to be carried out in a more rapid and efficient fashion than previously possible. Moreover, they allow for the preparation of new substances, which have previously been inaccessible. These new compounds have the possibility of having physiological properties of great importance in medicinal chemistry and the pharmaceutical industry.